Casticin (3’, 5-dihydroxy-3, 4’, 6, 7-tetramethoxyflavone) is an active compound isolated from roots, stems,leaves, fruits and seeds of a variety of plants. It is well known for its pharmacological properties and hasbeen utilized as an anti-hyperprolactinemia, anti-tumor, anti-inflammatory, neuroprotetective, analgesic andimmunomodulatory agent. Recently, the anticancer activity of casticin has been extensively investigated. Theresulkts showed that it exerts protective potential by targeting apoptosis, considered important for cancertherapies. In this article, our aim was to review the pharmacological and therapeutic applications of casticinwith specific emphasis on its anticancer functions and related molecular mechanisms. Chemotherapeutic effectsare dependent on multiple molecular pathways, which may provide a new perspective of casticin as a candidateanti-neoplastic drug. This review suggests that additional studies and preclinical trials are required to determinespeciﬁc intracellular sites of action and derivative targets in order to fully understand the mechanisms of itsantitumor activity and validate this compound as a medicinal agent for the prevention and treatment of variouscancers.